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ADRENOCORTICOSTEROIDS

• Major categories of action: • Glucocorticoids: affecting intermediary metabolism

& resistance to stress• Mineralocorticoids: regulation of salt & water

retention • Corticosteroids with:

• androgenic activity • estrogenic activity

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• Major glucocorticoid: Cortisol • Major mineralocorticoid: Aldosterone • Major androgen: Dehydroepiandrosterone

(DHEA)

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AdrenocorticosteriodsShort acting • Cortisone , Hydrocortisone

Intermediate acting• Prednisone ( ORAL ),Prednisolone, • Methylprednisolone• Triamcinolone

Long acting• Dexamethasone, Betamethasone, Paramethasone

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Actions

• Metabolism – increases plasma glucose• stress hormone• Blood cells : decreases

• Lymphocytes• Monocytes• Eosinophils, basophils

• Immune suppression • Anti inflammatory action

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Others

• Stimulates gastrin secretion

• Osteoporosis

• Myopathy

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Clinical UsesDiagnosis of adrenal function, i.e • Dexamethasone suppression test – Cushings

syndromeTreatment of • Adrenal function disorders – Addison's disease • Inflammatory/immunological disorders (at higher

doses) • Rheumatoid arthritis , osteoarthritis• Allergic reactions• Bronchial asthma• Acceleration of lung maturation

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Special considerations

• During illness - specially if fever is present

Supplemental fludrocortisone (mineralocorticoid) • Strenuous exercise with sweating • During very hot weather • Gastrointestinal upsets

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Glucocorticoid Toxicity • Metabolic Effects

• iatrogenic Cushing's syndrome • moon facies • fat redistribution; e.g. truncal obesity • acne • hirsuitism • insomnia, increased appetite • weight gain • muscle wasting • skin thinning, bruising • hyperglycemia • osteoporosis, • Impaired wound healing

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Other Effects• Peptic ulcer development • Myopathy• Nausea, dizziness, weight loss• Subcapsular cataracts • Increased intraocular pressure/glaucoma • Psychosis (large dose corticosteroids) • Benign intracranial hypertension

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MINERALOCORTICOIDS

• Sodium/fluid retention • Potassium loss-- hypokalemia • Hypochloremic alkalosis • Hypertension

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CI - Adrenocorticosteriods

• Peptic ulcer disease • Heart disease/hypertension with congestive

heart failure • Psychoses • Diabetes • Osteoporosis • Glaucoma

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Antagonists of Adrenocortical AgentsMetyrapone: • selective inhibitor of steroid synthesis

• Use - Cushing's syndrome

Major adverse effects: • Salt and water retention • Hirsuitism

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Aminoglutethimide: • Blocks cholesterol to pregnenolone

conversion • Uses ; malignancies of Adrenal cortex• + Dexamethasone : Breast Ca

Ketoconazole: antifungal imidazole • Use - Cushing's disease

Mifepristone : anti glucocorticoid + anti progestin

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Anti Mineralocorticoids

Antagonist – Spironolactone• Competes for the receptors• Inhibits Na reabsorption & prevents K

excretionUses• Hyperaldosteronism• Hirsutism in women• Diuretic